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Title: Discovery of novel halogenated 8-hydroxyquinoline-based anti-MRSA agents: In vitro and QSAR studies
Authors: Rungrot Cherdtrakulkiat
Apilak Worachartcheewan
Srisurang Tantimavanich
Ratana Lawung
Nujarin Sinthupoom
Supaluk Prachayasittikul
Somsak Ruchirawat
Virapong Prachayasittikul
Chulabhorn Research Institute
Mahidol University
Ministry of Education
Chulabhorn Graduate Institute
Keywords: Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-Feb-2020
Citation: Drug Development Research. Vol.81, No.1 (2020), 127-135
Abstract: © 2019 Wiley Periodicals, Inc. Methicillin-resistant Staphylococcus aureus (MRSA) infection has been considered to be one of global health problems due to limited classes of effective antimicrobial drugs. Herein, 8-hydroxyquinoline (8HQ) and its derivatives (1-7) were investigated for their anti-MRSA and antioxidant activities. Cloxyquin (2), a halogenated 8HQ, exerted the highest antimicrobial activity (MIC50 ≤ 5.57 μM) with high safety index, whereas an amino-derivative 7 showed the strongest antioxidant activity. Additionally, quantitative structure-activity relationship (QSAR) study demonstrated that mass, polarizability, topological charge, and van der Waals volume are essential properties governing the anti-MRSA activity. Taken together, cloxyquin was highlighted as a promising compound for further development as a novel anti-MRSA agent. QSAR findings would also benefit for further rational design of novel 8HQ-based compounds to combat the MRSA resistance.
ISSN: 10982299
Appears in Collections:Scopus 2020

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